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    Interleukin-1 beta converting enzyme inhibitors
    37.
    发明专利
    Interleukin-1 beta converting enzyme inhibitors 未知

    公开(公告)号：NZ528282A

    公开(公告)日：2005-05-27

    申请号：NZ52828299

    申请日：1999-03-19

    Applicant: VERTEX PHARMA

    Inventor： WANNAMAKER MARION W ,  BEMIS GUY W ,  CHARIFSON PAUL S ,  LAUFFER DAVID J ,  MULLICAN MICHAEL D ,  MURCKO MARK A ,  WILSON KEITH P ,  JANETKA JAMES W ,  DAVIES ROBERT J ,  GRILLOT ANNE-LAURE ,  SHI ZHAN ,  FORSTER CORNELIA J

    IPC: C07D207/273 ,  A61K31/47 ,  A61K38/00 ,  A61K38/03 ,  A61K38/04 ,  A61P5/48 ,  A61P7/00 ,  A61P9/00 ,  A61P17/00 ,  A61P19/00 ,  A61P19/08 ,  A61P19/10 ,  A61P25/00 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07D401/12 ,  C07K5/02 ,  C07K5/023 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/4427 ,  A61K31/4965 ,  A61K31/497 ,  C07D403/12 ,  C07D409/12 ,  C07D207/12 ,  C07D211/06

    Abstract: Compounds of formula I are described wherein; Y is formula (a) or (b); X is -C(R3)2- or -N (R3)- ; m is 0 or 1 R1 is -C(O)C(O)R8, -S(O)R8, -S(O)N(H)-R8, -C(O)C(O)N(H)R8, -C(O)CH=CHR8, -C(O)CH2OR8, -C(O)CH2N(H)R8, -S(O)N(R8)2, -C(O)C(O)N(R8)2, -C(O)CH2N(R8)2, -CH2-alkenyl-R8, or -CH2-alkynyl-R8; R2 is-H and each R3 is independently -H, an amino acid side chain, -R8, alkenyl-R9, or alkynyl-R9, or each R3 together with the atom to which they are bound forma 3 to 7 membered cyclic or heterocyclic ring system, or R2 and one R3 together with the atoms to which they are bound, form a 3 to 7 membered cyclic or heterocyclic ring system, wherein a hydrogen atom bound to any -alkyl, -cycloalkyl, aryl or -heteroaryl carbon atom or any nitrogen atom of the ring system can be optionally replaced; R4 is H and each R5 is -H an amino acid side chain, -R8, -alkenyl-R9 or alkenyl-R9 or R4 and one of R5 together with the atoms to which they are bound form a 3 to 7 membered cyclic or heterocyclic ring system, selected from formulas (i) to (ix) wherein a hydrogen atom bound to any -alkyl, -cycloalkyl, aryl or -heteroaryl carbon atom or any nitrogen atom of the ring system can be optionally replaced; R6 is-H; R7 is -OH,-OR8, or-N(H)OH; R8 is independently -alkyl, -cycloalkyl, -aryl, -heteroaryl, -heterocyclyl, -alkylcycloalkyl, -alkylaryl, -alkylheteroaryl, or -alkylheterocyclyl, wherein a hydrogen atom bound to any -alkyl, -cycloalkyl, aryl or -heteroaryl carbon atom or any nitrogen atom of the ring system can be optionally replaced; R9 is independently-aryl,-heteroaryl, cycloalkyl, or-heterocyclyl, wherein a hydrogen atom bound to any -alkyl, -cycloalkyl, aryl or -heteroaryl carbon atom or any nitrogen atom of the ring system can be optionally replaced; R10 is independently -OH, -SH, -F, -Cl, -Br, -I, -NO2, -CN, -NH2, -CO2H, -C(O)NH2, -N(H)C(O)H, -N(H)C(O)NH2, -perfluoroalkyl, -O-alkyl, -O-aryl, -O-alkylaryl, -N(H)alkyl, -N(H)aryl, -N(H)-alkylaryl, -N(alkyl)2, -C(O)N(H)alkyl, -C(O)N(alkyl)2, -N(H)C(O)alkyl, -N(H)C(O)N(H)alkyl, N(H)C(O)N(alkyl)2, -S-alkyl, -S-aryl, -S-alkylaryl, -S(O)2alkyl,-S(O)alkyl,-C(O)alkyl, -CH2NH2, -CH2N(H)alkyl, -CH2N(alkyl)2, -alkyl, -cycloalkyl, -aryl, -heteroaryl, -heterocyclyl, -alkylcycloalkyl, -alkylaryl, -alkylheteroaryl, or -alkylheterocyclyl, wherein a hydrogen atom bound to any-aryl, -heteroaryl or nitrogen atom is optionally replaced; R11 is independently -OH, -SH, -F, -Cl, -Br, -I, -NO2, -CN, -NH2,-CO2H, -C(O)NH2, -N(H)C(O)H, -N(H)C(O)NH2, -alkyl, -cycloalkyl, -perfluoroalkyl, -O-alkyl, -O-aryl, -O-alkylaryl, -N(H)alkyl, -N(H)aryl, -N(H)-alkylaryl, -N(alkyl)2, -C(O)N(H)alkyl, -C(O)N(alkyl)2, -N(H)C(O)alkyl, -N(H)C(O)N(H)alkyl, -N(H)C(O)N(alkyl)2, -S-alkyl, -S-aryl, -S-alkylaryl, -S(O)2alkyl, -CH2NH2, -C(O)alkyl, -CH2N(H)alkyl, or-CH2N(alkyl)2. The compounds can be used in medicament for inhibiting ICE-mediated function and decreasing IGIF or IFN-gamma production and for treating disorders such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, or multiple myeloma. (62) Divided out of 506963

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